PD 123319 二(三氟乙酸盐)

更新时间:2019-03-28 14:14:56

PD 123319 二(三氟乙酸盐)结构式
PD 123319 二(三氟乙酸盐)
常用名 PD 123319 二(三氟乙酸盐) 英文名 PD 123319 ditrifluoroacetate
CAS号 136676-91-0 分子量 736.657
密度 N/A 沸点 N/A
分子式 C35H34F6N4O7 熔点 N/A
MSDS N/A 闪点 N/A
符号 GHS07
GHS07
信号词 Warning

 PD 123319 二(三氟乙酸盐)用途


PD 123319 ditrifluoroacetate 是一种有效的,选择性的 AT2 angiotensin II receptor 拮抗剂,IC50 值为 34 nM。
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 PD 123319 二(三氟乙酸盐)名称

中文名 PD 123319 二(三氟乙酸盐)
英文名 PD 123319 bistrifluoroacetate
英文别名 更多

 PD 123319 二(三氟乙酸盐)生物活性

描述 PD 123319 ditrifluoroacetate 是一种有效的,选择性的 AT2 angiotensin II receptor 拮抗剂,IC50 值为 34 nM。
相关类别
靶点

IC50: 34 nM (AT2 Receptor)[1]

体外研究 PD 123319显示出在许多不同组织中区分AII受体的两个亚类。 125I-AII在牛肾上腺肾小球细胞的膜制剂中特异性标记AII的两类结合位点。第一类(DuP-753敏感)代表AII总结合位点的约85%,并且对DuP-753具有高亲和力(IC50为92.9nM)。 PD-123319对125I-AII与该位点的结合没有任何影响。第二类结合位点对PD-123319更敏感,IC50为6.9 nM,对DuP-753的亲和力低得多(IC50约为10 microM)[2]。
溶解度
体外:

H 2 O:≥36mg / mL(48.87 mM)

* “≥”表示可溶,但饱和度未知。

储备液
1 mM 1.3575 mL 6.7874 mL 13.5748 mL
5 mM 0.2715 mL 1.3575 mL 2.7150 mL
10 mM 0.1357 mL 0.6787 mL 1.3575 mL
存储

4°C,在氮气下储存

运输 室温;可能会有所不同
SMILES FC(F)(C(O)=O)F.FC(F)(C(O)=O)F.O=C([C@@H]1CC2=C(N=CN2CC3=CC=C(N(C)C)C(C)=C3)CN1C(C(C4=CC=CC=C4)C5=CC=CC=C5)=O)O
参考文献

[1]. Blankley CJ, et al. Synthesis and structure-activity relationships of a novel series of non-peptide angiotensin II receptor binding inhibitors specific for the AT2 subtype. J Med Chem. 1991 Nov;34(11):3248-60.

[2]. Boulay G, et al. Modulation of angiotensin II binding affinity by allosteric interaction of polyvinyl sulfate with an intracellular domain of the DuP-753-sensitive angiotensin II receptor of bovine adrenal glomerulosa. Mol Pharmacol. 1992 Apr;41(4):809-15

[3]. Estrup TM, et al. No effect of angiotensin II AT(2)-receptor antagonist PD 123319 on cerebral blood flow autoregulation. J Renin Angiotensin Aldosterone Syst. 2001 Sep;2(3):188-92.

[4]. Brillante DG, et al. Effects of intravenous PD 123319 on haemodynamic and arterial stiffness indices in healthy volunteers. J Renin Angiotensin Aldosterone Syst. 2005 Sep;6(2):102-6.

相关活性
小分子
血管紧张素II | AVE 0991 | A 779 | 曲尼斯特 | 替米沙坦 | CGP-42112 | LCZ696 | 奥洛立更 | 非马沙坦 | 血管紧张素 | Sparsentan | C型利钠肽(CNP)(1-22),人 | BIBS 39
相关文档

SDS |COA |HNMR |LCMS

*以上文档由Medchemexpress提供,仅用于科学研究参考。

 PD 123319 二(三氟乙酸盐)物理化学性质

分子式 C35H34F6N4O7
分子量 736.657
精确质量 736.233154
PSA 115.97000
LogP 5.04700

 PD 123319 二(三氟乙酸盐)安全信息

符号 GHS07
GHS07
信号词 Warning
危害声明 H315-H319-H335
警示性声明 P261-P305 + P351 + P338
个人防护装备 dust mask type N95 (US);Eyeshields;Gloves
危险品运输编码 NONH for all modes of transport

 PD 123319 二(三氟乙酸盐)文献5

更多文献
Contractility of placental vascular smooth muscle cells in response to stimuli produced by the placenta: roles of ACE vs. non-ACE and AT1 vs. AT2 in placental vessel cells.

Placenta 29(6) , 503-9, (2008)

Our previously published work has shown that non-ACE angiotensin II (Ang II) generating system is dominate in the placenta and may play a critical role in regulation of placental vascular contractile ...

Modulation of angiotensin II binding affinity by allosteric interaction of polyvinyl sulfate with an intracellular domain of the DuP-753-sensitive angiotensin II receptor of bovine adrenal glomerulosa.

Mol. Pharmacol. 41 , 809-815, (1992)

Angiotensin II (AII) is an important regulator of aldosterone secretion by adrenal glomerulosa cells. All interacts with a specific receptor coupled to a guanine nucleotide-binding protein that contro...

Differential blockade of central effects of angiotensin II by AT2-receptor antagonists.

Am. J. Physiol. 265 , H226, (1993)

In conscious, chronically instrumented, male Long-Evans rats, we showed previously that central administration (intracerebroventricular) of the AT1-receptor antagonist EXP-3174 (1 microgram) caused a ...

 PD 123319 二(三氟乙酸盐)英文别名

1H-Imidazo[4,5-c]pyridine-6-carboxylic acid, 1-[[4-(dimethylamino)-3-methylphenyl]methyl]-5-(2,2-diphenylacetyl)-4,5,6,7-tetrahydro-, (6S)-
(S)-1-<<4-(dimethylamino)-3-methylphenyl>methyl>-5-(diphenylacetyl)-4,5,6,7-tetrahydro-1H-imidazo<4,5-c>pyridine-6-carboxylic acid
(6S)-1-[4-(Dimethylamino)-3-methylbenzyl]-5-(diphenylacetyl)-4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridine-6-carboxylic acid trifluoroacetate (1:2)
S-(+)-1-[(4-(dimethylamino)-3-methylphenyl)methyl]-5-(diphenylacetyl)-4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridine-6-carboxylic acid di(trifluoroacetate)
1H-Imidazo[4,5-c]pyridine-6-carboxylic acid, 1-[[4-(dimethylamino)-3-methylphenyl]methyl]-5-(2,2-diphenylacetyl)-4,5,6,7-tetrahydro-, (6S)-, compd. with 2,2,2-trifluoroacetic acid (1:2)
(3S)-9-[(4-DIMETHYLAMINO-3-METHYL-PHENYL)METHYL]-4-(2,2-DIPHENYLACETYL)-4,7,9-TRIAZABICYCLO[4.3.0]NONA-7,10-DIENE-3-CARBOXYLIC ACID
1-((4-(Dimethylamino)-3-methylphenyl)methyl)-5-(diphenylacetyl)-4,5,6,7-tetrahydro-1H-imidazo[4.5-c]pyridine-6-carboxyli
PD 123,319 DITRIFLUOROACETATE
pd 123,319 di(trifluoroacetate) salt
1H-Imidazo(4,5-c)pyridine-6-carboxylic acid, 1-((4-(dimethylamino)-3-methylphenyl)methyl)-5-(diphenylacetyl)-4,5,6,7-tetrahydro-, (S)-
S-(+)-1-((4-(dimethylamino)-3-methylphenyl)methyl)-5-(diphenylacetyl)-4,5,6,7-tetrahydro-1H-imidazol(4,5-c)pyridine-6-carboxylic acid
(S)-1-((4-(dimethylamino)-3-methylphenyl)methyl)-5-(diphenylacetyl)-4,5,6,7-tetrahydro-1H-imidazo(4,5-c)pyridine-6-carboxylic acid,difluoroacetate salt
(6S)-1-[4-(Dimethylamino)-3-methylbenzyl]-5-(diphenylacetyl)-4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridine-6-carboxylic acid
(S)-1-{[4-(dimethylamino)-3-methylphenyl]methyl}-5-(diphenylacetyl)-4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridine-6-carboxylic acid
PD 123,319
(S)-1-{[4-(dimethylamino)-3-methylphenyl]methyl}-5-(diphenylacetyl)-4,5,6,7-tetrahydro-1H-imidazo-[4,5-c]pyridine-6-carboxylic acid,ditrifluoroacetate,dihydrate
PD 123319 (ditrifluoroacetate)
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参考价格:$186/10mM*1mLinWater

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